CAY10603

別名: BML-281

目錄號：S7596 Purity: 99.85%

CAY10603 (BML-281)是一種強(qiáng)效的選擇性HDAC6抑制劑，IC50為2 pM，選擇性比其它HDACs高200多倍。

CAY10603 Chemical Structure

CAS: 1045792-66-2

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1367.73	現(xiàn)貨
5mg	1181.73	現(xiàn)貨
25mg	3898.21	現(xiàn)貨
100mg	8177.36	現(xiàn)貨
1g	24488.1	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次： S759601 DMSO]89 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false 純度： 99.85%

99.85

CAY10603相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	點(diǎn)擊展開
相關(guān)產(chǎn)品	Entinostat (MS-275) TSA (Trichostatin A) Mocetinostat (MGCD0103) RGFP966 Tubastatin A Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) 2HCl MC1568 Tubastatin A HCl PCI-34051 Tacedinaline (CI994) LMK-235 Fimepinostat (CUDC-907) Tubacin Givinostat hydrochloride monohydrate AR-42 TMP269 Sodium butyrate Pracinostat (SB939) Abexinostat (PCI-24781) CUDC-101 Santacruzamate A (CAY10683) (-)-Parthenolide Dacinostat (LAQ824) RG2833 (RGFP109) Tasquinimod Tucidinostat (Chidamide) TMP195 Nexturastat A Droxinostat Domatinostat (4SC-202) Scriptaid 4-PBA (4-Phenylbutyric acid) M344 Resminostat BG45 Citarinostat (ACY-241) ACY-738 WT161 HPOB ITSA-1 (ITSA1) TC-H 106 SIS17 Tubastatin A TFA Raddeanin A TH34 BML-210 (CAY10433) ACY-775	點(diǎn)擊展開
相關(guān)化合物庫	FDA藥物庫天然產(chǎn)物庫凋亡分子化合物庫 DNA損傷/ DNA修復(fù)化合物庫細(xì)胞周期化合物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)信息(PMID)
human SU.86.86 cells	Proliferation assay	72 h	Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay, IC50=0.6 μM	18642892
HPDE 6c7 cells	Cytotoxicity assay	72 h	Cytotoxicity against HPDE 6c7 cells after 72 hrs by MTT assay, IC50=0.5 μM	18642892
human HupT3 cells	Proliferation assay	72 h	Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay, IC50=0.3 μM	18642892
human MiaPaca2 cells	Proliferation assay	72 h	Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay, IC50=0.1 μM	18642892
human Panc04.03 cells	Proliferation assay	72 h	Antiproliferative activity against human Panc04.03 cells after 72 hrs by MTT assay, IC50=0.1 μM	18642892
human BxPC3 cells	Proliferation assay	72 h	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay, IC50=1 μM	18642892
HMEC	Cytotoxicity assay	72 h	Cytotoxicity against HMEC after 72 hrs by MTT assay, IC50=1 μM	18642892
sf9	Function assay	5 to 10 mins	Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins, IC50=0.0032μM.	31414801
sf9	Function assay	5 to 10 mins	Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins, IC50=0.0138μM.	31414801
HeLa	Function assay	2 hrs	Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay, IC50=0.79433μM.	30964290
MV4-11	Function assay	1 hr	Binding affinity to HDAC6 in human MV4-11 cells assessed as increase in cellular protein stabilization at 1 uL preincubated for 1 hr followed by heating at 52 degree C for 3.5 mins by CETSA	32212730
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

CAY10603 (BML-281)是一種強(qiáng)效的選擇性HDAC6抑制劑，IC50為2 pM，選擇性比其它HDACs高200多倍。

靶點(diǎn)

HDAC6 ^[1]
(Cell-free assay)

2 pM

體外研究(In Vitro)
體外研究活性	CAY10603，通過抑制HDAC6，對胰腺癌細(xì)胞系表現(xiàn)出有效的抗增殖活性，IC50 <1 μM，其可以用作新的分子探針以探索HDAC的生物學(xué)性能。^[1]
激酶實(shí)驗(yàn)	HDAC 抑制試驗(yàn)
激酶實(shí)驗(yàn)	純化的HDACs與1 mM羧基熒光素(FAM)-標(biāo)記的乙酰化多肽底物和測試化合物在HDAC試驗(yàn)緩沖液中于25℃下培養(yǎng)17小時(shí)，試驗(yàn)緩沖液包含100 mM HEPES (pH 7.5)，25 mM KCl，0.1% BSA，和0.01% Triton X-100。加入包含0.078% SDS的緩沖液(終SDS濃度為0.05%)終止反應(yīng)。底物和產(chǎn)物使用Caliper LabChip 3000系統(tǒng)電泳分離，以藍(lán)色激光激發(fā)，綠色熒光檢測(CCD2)。底物和產(chǎn)品峰的熒光強(qiáng)度使用Well Analyzer軟件在Caliper系統(tǒng)中檢測。對每個(gè)樣品，反應(yīng)重復(fù)進(jìn)行兩次。IC50值使用Microsoft Excel 中IDBS XLFit版4.2.1 插件和XLFit 4參數(shù)Logistic模型: ((A+((B_A)/1+((C/x)D))))自動計(jì)算，公式中X是化合物濃度，A和B分別為估計(jì)的最小和最大抑制百分比，C是拐點(diǎn)，D是S形曲線的Hill斜率。IC50的標(biāo)準(zhǔn)差使用Microsoft Excel 中IDBS XLFit版4.2.1 插件和公式xf4_FitResultStdError自動計(jì)算。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	BxPc-3，HupT3，Mia Paca-2，Panc 04.03，和 SU 86.86 細(xì)胞
	濃度	~50 μM
	孵育時(shí)間	72小時(shí)
	方法	胰腺癌細(xì)胞系BxPc-3，HupT3，Mia Paca-2，Panc 04.03，和SU 86.86在包含10%胎牛血清和左旋谷酰胺的培養(yǎng)基(DMEM或RPMI)中生長。胰腺癌細(xì)胞重復(fù)兩份接種在96孔板的6孔中。接種4小時(shí)后，各孔用稀釋劑(DMSO)或不同濃度的SAHA或指示的1 nM到50 mM濃度的HDACIs進(jìn)行處理。細(xì)胞毒性在處理后 “0”，和 72 小時(shí)使用比色MTT法根據(jù)制造商的建議進(jìn)行測量。IC50值使用XLfit計(jì)算。

參考文獻(xiàn)
https://pubmed.ncbi.nlm.nih.gov/18642892/

參考文獻(xiàn)

https://pubmed.ncbi.nlm.nih.gov/18642892/

化學(xué)信息&溶解度

分子量	446.5	分子式	C₂₂H₃₀N₄O₆
CAS號	1045792-66-2	SDF	Download CAY10603 SDF
Smiles	CC(C)(C)OC(=O)NC1=CC=C(C=C1)C2=CC(=NO2)C(=O)NCCCCCCC(=O)NO
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 89 mg/mL ( (199.32 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 5 mg/mL (11.19 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解配方
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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操作手冊

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常見問題及建議解決方法

問題 1:
I want to use CAY10603 and Tubastatin A via IP for mice. What can serve as the working solution instead of DMSO?

回答：
S7596 CAY10603 can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 9mg/ml as a clear solution. The dissolving protocol is the same as S8049.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):